C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 1/107 (2006.01) C07K 14/575 (2006.01) C07K 14/605 (2006.01) C07K 14/62 (2006.01) C07C 235/70 (2006.01)
Patent
CA 2500123
The present invention provides a method for acylating one or more amino groups of a peptide where the acylation reaction is to be performed in an aqueous mixture containing less than 10 %w/w aprotic polar solvent. a) reacting the peptide having at least one free amino group with an acylating agent of the general formula I wherein n, is 0-8 R1is COOR4; R2 is a lipophilic moiety; R3 together with the carboxyl group to which R3 is attached designate a reactive ester or a reactive N-hydroxy imide ester; and R4 is selected from hydrogen, C1-12-alkyl and benzyl, under basic conditions in an aqueous mixture;
L'invention concerne un procédé d'acylation d'un ou de plusieurs groupes amino d'un peptide, procédé selon lequel la réaction d'acylation est effectuée dans un milieu aqueux contenant moins de 10 %(m/m) d'un solvant polaire aprotique.
Duenweber Dorte Lunoe
Hansen Louis Brammer
Jensen Inge Holm
Dimock Stratton Llp
Novo Nordisk A/s
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